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说明： Potent and selective CSN5 (COP9 signalosome) inhibitor
化学名： 3-(Difluoromethyl)-N-(6-((5S,6S)-6-hydroxy-6,7,8,9-tetrahydro-5H-imidazo[1,5-a]azepin-5-yl)-[1,10-biphenyl]-3-yl)-1-isopropyl-1H-pyrazole-5-carboxamide
纯度： ≥98% (HPLC)
生物活性 for CSN5i-3
CSN5i-3 is a potent and selective CSN5 (COP9 signalosome) inhibitor. It inhibits deneddylation of NEDD8-modifed CRLs (IC50 = 5.8 nM), keeping them in the neddylated state, and leading to inactivation of a subset of CRLs by inducing degradation of their substrate receptor module (SRM). In A2780 ovarian cancer cells, CSN5i-3 down-regulates the expression of COPS5 and arrest cells at S-phase. In HUVECs in vitro and in zebrafish embryos in vivo, CSN5i-3 induces endothelial barrier disruption and increases macromolecule leakage by increasing the expression and activity of RhoGTPases. CSN5i-3 also inhibits the growth of lymphoma cell xenografts in mice. Orally bioavailable.
The negative control CSN5i-3-NEG (Cat. No. 7532) is also available.
Scientific Data
Novartis vs Bio-Techne batch comparison for CSN5i-3 Effects of CSN5i-3 on a cancer cell line. (A) Concentration dependent effects (t = 3 days) of CSN5i-3. The IC50 values are 26 nM and 16 nM for Novartis batch and Bio-Techne batch, respectively. (B) Cullins Cul4A level after treatment (t = 2 hours) with 100 nM of CSN5i-3 from either Novartis or Bio-Techne.
技术数据 for CSN5i-3
| 分子量 | 505.57 |
| 公式 | C28H29F2N5O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2375740-98-8 |
| PubChem ID | 129892190 |
| InChI Key | ANNKHJQLDMGQFM-UIOOFZCWSA-N |
| Smiles | CC(N1N=C(C(F)F)C=C1C(NC2=CC(C3=CC=CC=C3)=C([C@H]4[C@H](CCCC5=CN=CN45)O)C=C2)=O)C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for CSN5i-3
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 50.56 | 100 |
制备储备液 for CSN5i-3
以下数据基于产品分子量 505.57。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.98 mL | 9.89 mL | 19.78 mL |
| 5 mM | 0.4 mL | 1.98 mL | 3.96 mL |
| 10 mM | 0.2 mL | 0.99 mL | 1.98 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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产品说明书 for CSN5i-3
参考文献 for CSN5i-3
参考文献是支持产品生物活性的出版物。
Schlierf et al (2016) Targeted inhibition of the COP9 signalosome for treatment of cancer. Nat.Commun. 7 13166 PMID: 27774986
Zhange et al (2017) COPS5 inhibition arrests the proliferation and growth of serous ovarian cancer cells via the elevation of p27 level. Biochem.Biophys.Res.Commun. 493 85 PMID: 28919423
Majolée et al (2019) CSN5 inhibition triggers inflammatory signaling and Rho/ROCK-dependent loss of endothelial integrity. Sci.Rep. 9 9131 PMID: 31148579
If you know of a relevant reference for CSN5i-3, please let us know.
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关键词: CSN5i-3, CSN5i-3 supplier, CSN5I3, potent, selective, inhibitors, inhibits, CSN5, COP9, signalosome, antitumour, antitumor, constitutive, photomorphogenesis, 9, NEDD8, neddylation, cullin-ring, CRL, Rho, GTPases, expression, activation, activators, Ubiquitin, E3, Ligases, 7089, Tocris Bioscience
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There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
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Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia